Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Amrita Ágnes, Bobok"'
Autor:
József, Huszár, József Levente, Petró, Zsuzsa, Hadady, Amrita Ágnes, Bobok, Katalin, Sághy, Attila Sándor, Halász, Gábor, Hornyánszky, Viktor, Román, István, Greiner, János, Éles
Publikováno v:
Bioorganicmedicinal chemistry letters. 67
The systemic use of GABA
Autor:
József Huszár, József Levente Petró, Zsuzsa Hadady, Amrita Ágnes Bobok, Katalin Sághy, Attila Sándor Halász, Gábor Hornyánszky, Viktor Román, István Greiner, János Éles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 67:128714
Autor:
Istvan Laszlovszky, András Visegrády, Balázs Krámos, Viktor Román, Balázs Lendvai, Bela Kiss, Amrita Ágnes Bobok, György Lévay
Publikováno v:
Biomolecules
Biomolecules, Vol 11, Iss 104, p 104 (2021)
Biomolecules, Vol 11, Iss 104, p 104 (2021)
Dopamine (DA), as one of the major neurotransmitters in the central nervous system (CNS) and periphery, exerts its actions through five types of receptors which belong to two major subfamilies such as D1-like (i.e., D1 and D5 receptors) and D2-like (
Autor:
Attila Sándor Halász, Amrita Ágnes Bobok, Zoltán Szakács, István Greiner, Zoltán Orgován, Mónika Vastag, Sándor Kolok, Zoltán Béni, Gábor Wágner, Mónika L. Mikó-Bakk, Zsolt Szombathelyi, Attila Bielik, Krisztina Gál, Katalin Nogradi, György M. Keserű, Ottilia Balázs, Katalin Saghy, János Kóti, György T. Balogh, Judit Laszy, Mikhail Krasavin, György Domány, Janos Galambos
Publikováno v:
Journal of Medicinal Chemistry. 60:2470-2484
Negative allosteric modulators (NAM) of metabotropic glutamate receptor 5 (mGluR5) have been implicated as a potential pharmacotherapy for a number of psychiatric diseases, including anxiety and depression. Most of the mGluR5 NAM clinical candidates
Autor:
Áron Szigetvári, Mónika Vastag, Katalin Saghy, Zoltán Orgován, Zoltán Béni, Attila Bielik, István Greiner, Zsuzsanna Sánta, György Domány, Janos Galambos, Amrita Ágnes Bobok, Mikhail Krasavin, Zsolt Szombathelyi, János Kóti, Gábor Wágner, Mónika L. Mikó-Bakk, Krisztina Gál, György M. Keserű, Bela Kiss
Publikováno v:
European Journal of Medicinal Chemistry, 133, 240-254. Elsevier Masson SAS
Galambos, J, Bielik, A, Wágner, G, Domány, G, Kóti, J, Béni, Z, Szigetvári, Á, Sánta, Z, Orgován, Z, Bobok, A, Kiss, B, Mikó-Bakk, M L, Vastag, M, Sághy, K, Krasavin, M, Gál, K, Greiner, I, Szombathelyi, Z & Keserű, G M 2017, ' Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu 5 ) receptor negative allosteric modulators ', European Journal of Medicinal Chemistry, vol. 133, pp. 240-254 . https://doi.org/10.1016/j.ejmech.2017.03.071
Galambos, J, Bielik, A, Wágner, G, Domány, G, Kóti, J, Béni, Z, Szigetvári, Á, Sánta, Z, Orgován, Z, Bobok, A, Kiss, B, Mikó-Bakk, M L, Vastag, M, Sághy, K, Krasavin, M, Gál, K, Greiner, I, Szombathelyi, Z & Keserű, G M 2017, ' Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu 5 ) receptor negative allosteric modulators ', European Journal of Medicinal Chemistry, vol. 133, pp. 240-254 . https://doi.org/10.1016/j.ejmech.2017.03.071
Negative allosteric modulators of metabotropic glutamate receptor 5 (mGlu5) showed efficacy in a number of animal models of different CNS diseases including anxiety and depression. Virtually all of the compounds which reached the clinic belong to the
Autor:
Katalin Fónagy, Krisztina Gál, Sándor Farkas, György M. Keserű, Ildikó Magdó, Bela Kiss, Gábor Wágner, Katalin Nogradi, Zsolt Szombathelyi, Sándor Kolok, Viktor Háda, János Kóti, Amrita Ágnes Bobok, Istvan Gyertyan, István Greiner, György Domány
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3845-3849
An HTS campaign of our corporate compound library resulted in thieno[2,3-b]pyridines derivative hits with mGluR5 negative allosteric modulator effects. During the hit-to-lead development our objective was to improve affinity, and to keep the ligand e
Autor:
Amrita Ágnes Bobok, György Domány, Zoltán Szakács, Krisztina Gál, Katalin Saghy, György M. Keserű, Katalin Nogradi, Zsolt Szombathelyi, Sándor Kolok, Janos Galambos, János Kóti, Zoltán Béni, István Greiner, Gábor Wágner, Mónika L. Mikó-Bakk, Mónika Vastag
Publikováno v:
Galambos, J, Domány, G, Nógrádi, K, Wágner, G, Keseru, G M, Bobok, A, Kolok, S, Mikó-Bakk, M L, Vastag, M, Sághy, K, Kóti, J, Szakács, Z, Béni, Z, Gál, K, Szombathelyi, Z & Greiner, I 2016, ' 4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors : From HTS hit to development candidate ', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1249-1252 . https://doi.org/10.1016/j.bmcl.2016.01.024
Bioorganic and Medicinal Chemistry Letters, 26(4), 1249-1252. Elsevier Limited
Bioorganic and Medicinal Chemistry Letters, 26(4), 1249-1252. Elsevier Limited
High throughput screening of our corporate compound library followed by hit-to-lead development resulted in a 4-aryl-3-arylsulfonyl-quinoline derivative lead (2) with mGluR5 negative allosteric modulator activity. During the lead optimization process
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34b9293cfa61b23617d4ae5ab3c9f312
https://research.vu.nl/en/publications/90c75f64-ce57-4f0f-aa17-4c3a16a1765e
https://research.vu.nl/en/publications/90c75f64-ce57-4f0f-aa17-4c3a16a1765e
Publikováno v:
Synapse. 65:467-478
In vitro binding characteristics of the dopamine D₃/D₂ antagonist [³H]raclopride were compared to the D₃/D₂ agonist [³H](+)-PHNO in membrane preparations from rat striatum, cerebellum Lobules 9 and 10 (CB L9,10), and other cerebellar region
Autor:
András Visegrády, Sándor Kolok, Márton Vass, Dalma Kurkó, György M. Keserű, Edit Szőllősi, László Kiss, Amrita Ágnes Bobok
Publikováno v:
Bioorganicmedicinal chemistry. 23(14)
Fragment-based drug discovery has emerged as an alternative to conventional lead identification and optimization strategies generally supported by biophysical detection techniques. Membrane targets like G protein-coupled receptors (GPCRs), however, o
Autor:
Attila Bielik, Dalma Kurkó, Istvan Gyertyan, Gábor Wágner, Mónika Vastag, Krisztina Gál, Attila Horváth, Bela Kiss, György M. Keserü, Sándor Kolok, László Molnár, Zsolt Szombathelyi, József Nagy, Katalin Saghy, Amrita Ágnes Bobok, György Domány, Mónika L Bakk, Katalin Nogradi, István Greiner, Janos Galambos
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(15)
Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of this class of compounds was successfully eliminated. Systematic exploration of different p